Spray-dried Cefixime Encapsulated Poly(lactide-co-glycolide) Microparticles: Characterization and Evaluation of In Vitro Release Kinetics with Antibacterial Activity

Abstract

Our study reports on the development of novel biodegradable microparticles prepared by a spray-drying technique using the poly(lactide-co-glycolide) (PLGA), a biodegradable polymer for the controlled delivery of cefixime. Cefixime is a water-soluble drug having short biological half-life of 3 h. The behavior of PLGA in controlling drug release responses of cefixime microparticles was investigated. The resultant microparticles were characterized by scanning electron microscopy, encapsulation efficiency, particle-size distribution, X-ray diffraction, and in vitro dissolution studies (pH 7.2). To investigate the type of release mechanism that occurs, dissolution data were plotted according to different kinetic models. The in vitro release profiles from microparticles followed first order and Higuchi model release. Antibacterial studies were carried out using a standard agar diffusion method to determine the effectiveness of formulations in inhibiting the growth of microorganisms. It showed that the released drug from the formulations was effectively inhibiting the growth of microorganisms with the minimum inhibitory concentration of < 1 µg/mL. Data revealed the potential of formulations for treatment of infections caused by various microorganisms. Thus, this study demonstrates the high potential of the spray-drying technique to obtain stable cefixime microparticles with good encapsulation efficiency to achieve a delivery profile that would yield the controlled released level of the drug over a long period of time (74 h).

Keywords:

• Antibacterial activity
• Cefixime
• Controlled delivery
• Encapsulation
• Microparticles
• PLGA
• Spray drying technique

ACKNOWLEDGMENT

The authors thank SICART, Vallabh Vidyanagar, Anand, Gujarat, India, for analytical characterization and Charutar Vidyamandal (CVM) for providing all the research facilities.

Notes

A. E. coli.

B. S. aureus.

C. P. aeruginosa.

D. K. Pneumoniae.

A1 - 4% PLGA +15% Cefixime, A2 – 4% PLGA +20% Cefixime.

*0, no zone of inhibition.

*zone of inhibition of pure drug after 12 h was 2.6 (E. coli) and 4.6 (K. pneumonia).